The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: saturable and reversible binding to rat cortex membranes

Eur J Pharmacol. 1992 Jul 7;217(2-3):203-5. doi: 10.1016/0014-2999(92)90851-t.


We describe the binding to rat cortex membranes of [125I]iodophenpropit, the first radiolabeled histamine H3 antagonist. The binding of [125I]iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM; Bmax 209 fmol/mg of protein). Specific binding at a concentration of 0.3 nM accounted for 45-55% of the total binding. [125I]Iodophenpropit seems to fulfill the criteria for a suitable ligand for histamine H3 receptor binding studies.

MeSH terms

  • Animals
  • Binding Sites
  • Cerebral Cortex / metabolism*
  • Histamine Antagonists
  • Imidazoles / metabolism*
  • Iodine Radioisotopes
  • Isothiuronium / analogs & derivatives*
  • Isothiuronium / metabolism
  • Male
  • Rats
  • Rats, Wistar
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H3


  • Histamine Antagonists
  • Imidazoles
  • Iodine Radioisotopes
  • Receptors, Histamine
  • Receptors, Histamine H3
  • Isothiuronium
  • iodophenpropit